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Retaspimycin

Product Name
Retaspimycin
CAS No.
857402-23-4
Chemical Name
Retaspimycin
Synonyms
retamycin;retaspimycin;Unii-bzf2zm0I5z;18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propenylamino)geldanamycin;Geldanamycin, 18,21-didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)-
CBNumber
CB31518530
Molecular Formula
C31H45N3O8
Formula Weight
587.7
MOL File
857402-23-4.mol
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Retaspimycin Property

Boiling point:
800.9±65.0 °C(Predicted)
Density 
1.23
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
pka
10.15±0.70(Predicted)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ApexBio Technology
Product number
A3756
Product name
Retaspimycin
Packaging
5mg
Price
$175
Updated
2021/12/16
ApexBio Technology
Product number
A3756
Product name
Retaspimycin
Packaging
10mg
Price
$315
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0005299
Product name
RETASPIMYCIN
Purity
95.00%
Packaging
5MG
Price
$364.1
Updated
2021/12/16
ApexBio Technology
Product number
A3756
Product name
Retaspimycin
Packaging
50mg
Price
$795
Updated
2021/12/16
ApexBio Technology
Product number
A3756
Product name
Retaspimycin
Packaging
100mg
Price
$1395
Updated
2021/12/16
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Retaspimycin Chemical Properties,Usage,Production

Description

Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis.

Uses

Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.

Definition

ChEBI: An ansamycin that is tanespimycin in which the benzoquinone moiety has been reduced to the corresponding hydroquinone. A semi-synthetic analogue of geldanamycin, it is used (generally as the hydrochloride salt) in cancer treatment.

Biological Activity

IPI-504 potently inhibits proliferation in several tumor cell lines with 50% inhibition concentration IC50 values ranging from 10-40 nM and has been used for the treatment of gastrointestinal stromal tumors, soft-tissue sarcomas and non-small cell lung cancer.

target

HSP90

Mode of action

Cancer cells depend on the Hsp90 chaperone to maintain many proteins critical for cancer growth, proliferation and survival in a functional state. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which results in the induction of apoptosis.

References

[1]. hanson b e, vesole d h. retaspimycin hydrochloride (ipi-504): a novel heat shock protein inhibitor as an anticancer agent. 2009.
[2]. floris g, debiec-rychter m, wozniak a, et al. the heat shock protein 90 inhibitor ipi-504 induces kit degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors. molecular cancer therapeutics, 2011, 10(10): 1897-1908.

Retaspimycin Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Retaspimycin manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Retaspimycin 857402-23-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Retaspimycin 857402-23-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-08

857402-23-4, RetaspimycinRelated Search:


  • retaspimycin
  • 18,21-Didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propenylamino)geldanamycin
  • Unii-bzf2zm0I5z
  • Geldanamycin, 18,21-didehydro-17-demethoxy-18,21-dideoxo-18,21-dihydroxy-17-(2-propen-1-ylamino)-
  • retamycin
  • 857402-23-4
  • C31H45N3O8